Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., Maytansinoids, Etc.) Patents (Class 514/229.5)
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Patent number: 11939322Abstract: This invention relates to a method for manufacturing 9-ethyl-6,6-dimethyl-8-[4-(morpholin-4-yl)piperidin-1-yl]-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile, and is industrially preferable, allowing an objective substance to be obtained in high yield more safely and easily than the conventional method.Type: GrantFiled: September 3, 2019Date of Patent: March 26, 2024Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroki Serizawa, Akira Kawase, Hiroshi Fukuda, Naoto Hama
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Patent number: 11352357Abstract: The present invention relates to a medicament for treating or preventing a disease related to orexin receptor, especially orexin type 2 receptor, comprising a new compound having a urea structure or a pharmaceutically acceptable salt thereof as an active ingredient. In more detail, the present invention relates to a medicament for treating or preventing narcolepsy, idiopathic hypersomnia, hypersomnia, sleep apnea syndrome, etc.Type: GrantFiled: November 15, 2021Date of Patent: June 7, 2022Assignee: Sumitomo Dainippon Pharma Co., Ltd.Inventors: Eiji Ideue, Masafumi Komiya, Shoukou Lee, Shunichiro Uesugi, Yuta Funakoshi
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Patent number: 10851126Abstract: Disclosed are methods for the preparation of ligands for complexes, methods for preparing complexes and complexes having those ligands. Also provided is the use of a complex as a catalyst in a method of synthesis.Type: GrantFiled: September 11, 2015Date of Patent: December 1, 2020Assignee: Johnson Matthey Public Limited CompanyInventors: Roy Hogkinson, Vaclav Jurcik, Hans Guenter Nedden, Martin Wills
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Patent number: 10792305Abstract: Described are compositions of matter and protocols useful for treatment of neurological and other disorders associated with inflammatory activities. In some embodiments the invention provides means of modulating neuroinflammation through administration of noble gas containing compositions. In other aspects, the invention provides means of modulating stem cell compartments to enhance endogenous reparative activities or to synergize with existing treatments.Type: GrantFiled: June 23, 2016Date of Patent: October 6, 2020Assignee: Nobilis Therapeutics, Inc.Inventors: Thomas Ichim, Vlad Bogin
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Patent number: 10752628Abstract: The present invention includes compound and methods that are useful in treating certain cancers, such as synovial sarcomas.Type: GrantFiled: November 16, 2016Date of Patent: August 25, 2020Assignees: THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE, DANA-FARBER CANCER INSTITUTE, INC.Inventors: Cigall Kadoch, Enrique Garcia-Rivera, Micah Maetani, Stuart L. Schreiber
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Patent number: 10660933Abstract: Provided are compositions, methods and devices for prophylaxis and/or therapy of sexually transmitted bacterial infections that infect the female reproductive tract. The compositions methods and devices are used for intravaginal administration of compositions that contain a peptide agent known as PIK and/or a compound known as ML-7. Demonstrations of embodiments are provided for infection models that involve Neisseria gonorrhoeae.Type: GrantFiled: October 31, 2016Date of Patent: May 26, 2020Assignee: University of Maryland, College ParkInventor: Wenxia Song
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Patent number: 10259826Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: March 24, 2017Date of Patent: April 16, 2019Assignee: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Patent number: 10246467Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R7, A, V, W, X, Y, n, r and q are defined in claim 1, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.Type: GrantFiled: August 20, 2015Date of Patent: April 2, 2019Assignee: Boehringer Ingelheim International GmbHInventors: Juergen Ramharter, Joachim Broeker, Annika Gille, Andreas Gollner, Manuel Henry, Nina Kerres, Harald Weinstabl
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Patent number: 10167298Abstract: The present invention relates to novel Pseudopolymorphs of Compound A, compositions comprising at least one Pseudopolymorph of Compound A, and methods of using the Pseudopolymorphs of Compound A for preparing compositions useful for treating or preventing HCV infection in a patient, wherein Compound A has the structure.Type: GrantFiled: October 24, 2014Date of Patent: January 1, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Michael McNevin, Yong Liu, Ian Mangion, Alfred Lee, Joyce Stellabott, Benjamin D. Sherry, Gary Martin, Kung-I Feng, Scott Schultz, Ryan Cohen, Yanfeng Zhang
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Patent number: 10125148Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: February 19, 2014Date of Patent: November 13, 2018Assignee: ViiV HEALTHCARE UK (NO. 5) LIMITEDInventors: Timothy P. Connolly, Stanley D'Andrea, John F. Kadow, David R. Langley, B. Narasimhulu Naidu, Manoj Patel, Kevin Peese, Michael A. Walker, Zhongyu Wang, Zhizhen Barbara Zheng
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Patent number: 9956227Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.Type: GrantFiled: December 3, 2014Date of Patent: May 1, 2018Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: Kimberly Vanover, Peng Li, Sharon Mates, Robert Davis, Lawrence P. Wennogle
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Patent number: 9932353Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: February 13, 2015Date of Patent: April 3, 2018Assignee: ViiV HEALTHCARE UK (NO. 5) LIMITEDInventors: B. Narasimhulu Naidu, Manoj Patel
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Patent number: 9872866Abstract: The present disclosure provides compositions that include a nanoparticle and a compound that increases the biological activity of the vitamin D receptor (VDR) (e.g., a VDR agonist), and methods of using such compounds to increase retention or storage of vitamin A, vitamin D, and/or lipids by a cell, such as an epithelial or stellate cell. Such methods can be used to treat or prevent fibrosis.Type: GrantFiled: October 23, 2015Date of Patent: January 23, 2018Assignees: Salk Institute for Biological Studies, The University of SydneyInventors: Ning Ding, Michael Downes, Christopher Liddle, Ronald M. Evans
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Patent number: 9839641Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.Type: GrantFiled: November 16, 2016Date of Patent: December 12, 2017Assignee: Entasis Therapeutics LimitedInventors: Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Hauck, Fei Zhou
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Patent number: 9834566Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV integrase, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: February 13, 2015Date of Patent: December 5, 2017Assignee: ViiV HEALTHCARE UK (NO.5) LIMITEDInventors: John F. Kadow, B. Narasimhulu Naidu, Manoj Patel, Kevin Peese, Tao Wang, Zhiwei Yin, Zhongxing Zhang
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Patent number: 9808471Abstract: Nasal pharmaceutical formulations comprising a drug substance having a specific particle size distribution profile are disclosed herein. Such profile provides increased bioavailability, increased efficacy or prolonged therapeutic effect of the drug substance when administered intranasally. The formulations of the present invention may comprise one or more corticosteroids having a specific particle size distribution profile. In a preferred embodiment, the corticosteroid is fluticasone or a pharmaceutically acceptable derivative thereof for the treatment of one or more symptoms of rhinitis. Preferably, the drug substance is fluticasone propionate. The formulations herein may be provided as an aqueous suspension suitable for inhalation via the intranasal route.Type: GrantFiled: April 16, 2003Date of Patent: November 7, 2017Assignee: Mylan Specialty LPInventor: Imtiaz Chaudry
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Patent number: 9540394Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.Type: GrantFiled: October 13, 2015Date of Patent: January 10, 2017Assignee: Entasis Therapeutics LimitedInventors: Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Hauck, Fei Zhou
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Patent number: 9388166Abstract: The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) can be used as medicament.Type: GrantFiled: April 17, 2015Date of Patent: July 12, 2016Assignee: Hoffman-La Roche Inc.Inventors: Zhi Chen, Shawn David Erickson
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Patent number: 9321788Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.Type: GrantFiled: June 11, 2012Date of Patent: April 26, 2016Assignee: BASILEA PHARMACEUTICA AGInventors: Berangere Gaucher, Franck Hubert Danel, Tong Xie, Lin Xu
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Patent number: 9242998Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: GrantFiled: February 3, 2014Date of Patent: January 26, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Shuwen He, Xing Dai, Anandan Palani, Ravi Nargund, Zhong Lai, Nicolas Zorn, Dong Xiao, Qun Dang, Casey C. McComas, Peng Li, Xuanjia Peng, Richard Soll
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Patent number: 9187495Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.Type: GrantFiled: October 16, 2014Date of Patent: November 17, 2015Assignee: Entasis Therapeutics LimitedInventors: Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
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Publication number: 20150139915Abstract: Methods and compositions are described for reducing airway reactivity and the susceptibility to asthmatic bronchoconstriction that involve increasing sphingolipid content in airways and lungs of a mammalian subject.Type: ApplicationFiled: May 16, 2013Publication date: May 21, 2015Inventors: Stefan Worgall, Tilla S. Worgall
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Publication number: 20150057270Abstract: The invention provides prodrugs of DNA-reactive analogs of duocarmycin and CC-1065 anticancer agents, wherein a cyclic prodrug form, such as carbamate, thionocarbamate, or carbamimidate, can be hydrolyzed by the patient in vivo to yield a respective bioactive agent comprising a DNA-alkylating moiety and a binding/targeting moiety. The DNA-reactive moiety is a ?-spiro-cyclohexenone fused to a heterocyclyl group which can be produced by endogenous hydrolysis of a cyclic carbamate prodrug of the invention. The cyclic carbamate prodrug produces no residual byproduct during activation in vivo. Methods of synthesis and biological methods and data are also provided.Type: ApplicationFiled: March 26, 2013Publication date: February 26, 2015Inventor: Dale L. Boger
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Publication number: 20150025066Abstract: Compounds of the formula I in which A, L1, L2, X and Y have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis.Type: ApplicationFiled: December 18, 2012Publication date: January 22, 2015Applicant: Merck Patent GmbHInventors: Henry Yu, Lizbeth Celeste Deselm
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Publication number: 20150018298Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, Y1, Y2, or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Inventors: Mingzhe Ji, Scott E. Lazerwith, Hyung-Jung Pyun
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Patent number: 8927541Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.Type: GrantFiled: December 17, 2010Date of Patent: January 6, 2015Assignee: Basilea Pharmaceutica AGInventors: Bérangère Gaucher, Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin Xu
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Publication number: 20140364429Abstract: Provided are compounds antiviral compounds represented by formula Ia and Ib: that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.Type: ApplicationFiled: June 6, 2014Publication date: December 11, 2014Applicant: AB PHARMA LTD.Inventor: Zheng-Yun James ZHAN
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Patent number: 8906929Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: August 5, 2013Date of Patent: December 9, 2014Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Manoj Patel, Stanley D'Andrea, Zhizhen Barbara Zheng, Timothy P. Connolly, David R. Langley, Kevin Peese, Zhongyu Wang, Michael A. Walker, John F. Kadow
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Patent number: 8889671Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.Type: GrantFiled: January 21, 2014Date of Patent: November 18, 2014Assignee: AstraZeneca ABInventors: Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
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Patent number: 8871759Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: GrantFiled: March 25, 2010Date of Patent: October 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Craig A. Coburn, Steven W. Ludmerer, Kun Liu, Hao Wu, Richard Soll, Bin Zhong, Jian Zhu
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Publication number: 20140303155Abstract: The invention relates to pharmacology and medicine, more particularly to novel pharmaceutical compositions and pharmaceutical kits for treating bacterial infections, and to novel method for treating diseases caused by bacterial infections including tuberculosis. The pharmaceutical composition is disclosed comprising Rifamycin and interferon inducer in pharmacologically effective doses, and also pharmaceutical kit for treating diseases caused by bacterial and healthcare acquired infections, comprising pharmacologically effective doses of Rifamycin in the form of a tablet, a capsule or an injection, interferon inducer in the form of a tablet, a capsule or an injection, and instruction for administration of the components of this pharmaceutical kit.Type: ApplicationFiled: October 25, 2012Publication date: October 9, 2014Inventors: Alexandre Vasilievich Ivachtchenko, Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk
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Publication number: 20140303144Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: October 9, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvajit Chakravarty
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Publication number: 20140256717Abstract: There is provided compounds of formula I, wherein R1, R2a, R2b, R2c, X, Y, Z, R3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and/or mTOR) is desired and/or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds.Type: ApplicationFiled: May 18, 2012Publication date: September 11, 2014Applicant: Centro Nacional de Investigaciones Oncológicas (CNIO)Inventors: Joaquín Pastor Fernández, Rosa Maria Álvarez Escobar, Rosario Concepción Riesco Fagundo, Ana Belén García García, Antonio Rodríguez Hergueta, Jose Ignacio Martin Hernando, Carmen Blanco Aparicio, David Álvaro Cebrián Muñoz
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Publication number: 20140228353Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: August 14, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
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Publication number: 20140221356Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: December 19, 2013Publication date: August 7, 2014Inventors: Haolun JIN, Scott E. LAZERWITH, Teresa Alejandra TREJO MARTIN, Elizabeth M. BACON, Jeromy J. COTTELL, Zhenhong R. CAI, Hyung-Jung PYUN, Philip Anthony MORGANELLI, Mingzhe JI, James G. TAYLOR, Xiaowu CHEN, Michael R. MISH, Manoj C. DESAI
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Publication number: 20140221355Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, Z2, or Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: December 19, 2013Publication date: August 7, 2014Inventors: Scott E. LAZERWITH, Haolun JIN, Hyung-Jung Pyun
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Publication number: 20140213571Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: August 20, 2012Publication date: July 31, 2014Inventors: Nigel J. Liverton, Casey Cameron McComas, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Shuwen He, Xing Dai, Hong Liu, Zhong Lai, Clare London, Dong Xiao, Nicolas Zorn, Ravi Nargund
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Publication number: 20140206677Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.Type: ApplicationFiled: January 21, 2014Publication date: July 24, 2014Applicant: AstraZeneca ABInventors: Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
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Publication number: 20140206663Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: March 19, 2014Publication date: July 24, 2014Inventors: Jianfei Wang, Eric C. Breinlinger, Martine Barth, Michael M. Friedman, Fabrice Guillier, Maria A. Argiriadi, Jeremy Edmunds, Dominique Potin, Adrian D. Hobson, Wentao Wu, Dominique Bonafoux, Didier Thomas, Dawn M. George, Linlin Dai, Yang Zhang
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Publication number: 20140200209Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: March 14, 2014Publication date: July 17, 2014Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
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Publication number: 20140199264Abstract: The present invention relates to novel Tetracyclic Xanthene Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b and R2 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Xanthene Derivative, and methods of using the Tetracyclic Xanthene Derivatives for treating or preventing HCV infection in a patient.Type: ApplicationFiled: March 16, 2012Publication date: July 17, 2014Inventors: Craig A. Coburn, Stuart B. Rosenblum, Joseph A. Kozlowski, Richard Soll, Hao Wu, Bin Hu, Bin Zhong, Dahai Wang, Changmao Shen, Fei Sun
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Publication number: 20140163021Abstract: Candidate compounds for use in neuro-protection and repair in neurological disorders involving Tau dysfunction (including Alzheimer's disease) are identified from a direct interaction between proteins FKBP52 and Tau. The method for screening a drug for the prevention and treatment of neurological disorders involving Tau dysfunction includes determining the ability of a candidate compound, to modulate binding between a Tau polypeptide and a FKBP52 polypeptide, and selecting positively the candidate compound that modulates binding.Type: ApplicationFiled: December 18, 2013Publication date: June 12, 2014Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Etienne Baulieu, Beatrice Chambraud
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Patent number: 8748464Abstract: The present disclosure provides a method of increasing an immune response in an individual, the method involving administering to an individual in need thereof an inhibitor of SIRT1. The present disclosure provides a method of reducing an immune response, e.g., to treat chronic immune hyperactivity, the method generally involving administering to an individual in need thereof an activator of SIRT1. The present disclosure provides a method of modulating activation and differentiation of CD4+ T cells.Type: GrantFiled: July 16, 2010Date of Patent: June 10, 2014Assignee: The J. David Gladstone InstitutesInventors: Eric M. Verdin, Melanie Ott, Hye-Sook Kwon, Hyungwook Lim
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Publication number: 20140128371Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: ASTRAZENECA ABInventors: Kevin BARVIAN, Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
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Patent number: 8685965Abstract: Compounds of Formula (I), (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, L, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG, W, Y and Z are as described herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.Type: GrantFiled: September 29, 2009Date of Patent: April 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Donnette D. Staas, Ian M. Bell, Harold G. Selnick
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Publication number: 20140080821Abstract: Provided herein are benzopyrimido-pyrrolo-oxazine-dione (BPO) compounds and pyrimido-pyrrolo-quinoxalinedione (PPQ) compounds, and compositions comprising these compounds, that inhibit cystic fibrosis transmembrane conductance regulator (CFTR) mediated ion transport and that are useful for treating diseases and disorders associated with aberrantly increased CFTR chloride channel activity, such as polycystic kidney disease and secretory diarrheas. The compounds and compositions comprising the compounds described herein may be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.Type: ApplicationFiled: May 25, 2012Publication date: March 20, 2014Applicant: The Regents of the University of CaliforniaInventors: Alan S. Verkman, David S. Snyder
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Publication number: 20140072536Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.Type: ApplicationFiled: March 15, 2013Publication date: March 13, 2014Applicant: Board of Regents of the Nevada System of Higher Education On Behalf of the University of NevadaInventors: Ryan Wuebbles, Dean Burkin
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Publication number: 20140050783Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.Type: ApplicationFiled: October 30, 2013Publication date: February 20, 2014Applicant: INTRA-CELLULAR THERAPIES INC.Inventors: Sharon MATES, Allen FIENBERG, Lawrence P. WENNOGLE
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Publication number: 20140051692Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: August 5, 2013Publication date: February 20, 2014Inventors: B. Narasimhulu Naidu, Manoj Patel, Stanley D'Andrea, Zhizhen Barbara Zheng, Timothy P. Connolly, David R. Langley, Kevin Peese, Zhongyu Wang, Michael A. Walker, John F. Kadow
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Patent number: 8624003Abstract: This invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding agent. The method described in this invention is advantageous for preparation of stably-linked conjugates of cell binding agents, such as antibodies with effector or reporter groups. This conjugation method provides in high yields conjugates of high purity and homogeneity that are without inter-chain cross-linking and inactivated linker residues.Type: GrantFiled: June 3, 2010Date of Patent: January 7, 2014Assignee: ImmunoGen, Inc.Inventors: Brenda A. Kellogg, Rajeeva Singh, Ravi V. J. Chari